Skip to main content
. 2018 Mar 6;10:425–437. doi: 10.2147/CMAR.S88825

Table 3.

Pharmacologic activity of regorafenib, M-2, and M-5 in cellular kinase phosphorylation assays12,13

Kinase, cell line Regorafenib
(IC50 [nM/L]±SD)		 Metabolite M-2
(IC50 [nM/L]±SD)		 Metabolite M-5
(IC50 [nM/L]±SD)
VEGFR-2, NIH-3T3 40 30 20
TIE-2, CHO 31±9 66±35 180±0
c-KIT wild type, M07e 23 13 110
c-KITK642E, GIST882 17±4 4±2 N/A
BRAFV600E, RAT-1 69 21 27

Abbreviations: CHO, Chinese hamster ovary; GIST, gastrointestinal stromal tumors; IC50, inhibitory concentration; N/A, not available; TIE-2, tyrosine kinase with immunoglobulin and epidermal growth factor homology domain 2; VEGFR-2, vascular endothelial growth factor receptor 2.